Nicotinamide derivative (Aptinib), with a molecular formula being C24H23N5O and a chemical name of N-[4-(1-cyanocyclopentyl) phenyl]-2-(4-pyridylmethyl) amidogen-3-pyridineethanamine, is a molecularly targeted antitumor drug and is a typical small molecule vascular endothelial growth factor tyrosine kinase inhibitor that can be used to treat advanced non-small cell lung cancer, gastric cancer, liver cancer, breast cancer and the like. The Chinese invention patent CN101676267 discloses the preparation method and application of the nicotinamide derivatives mesylate (with molecular formula C24H23N5O.CH4O3S). The nicotinamide derivative mesylate (hereinafter referred to as “nicotinamide derivative mesylate solids with needle shape”) obtained according to the method described in CN 101676267 is an anhydrate, which has needle shape and of hygroscopicity. As is known to those skilled in the art, a highly hygroscopic solid is difficult to be made into formulations under pharmaceutical processing conditions, whereas solids with needle shape are very viscous and of poor flowability due to the large amount of static electricity. Accordingly, there is a need for a crystal form of the nicotinamide derivative mesylate with superior physicochemical properties, which can be advantageously used in pharmaceutical processing and pharmaceutical compositions.
As we all know, the stability and bioavailability of different crystal forms of the same drug may be significantly different, thus affecting the efficacy of drug. Therefore, it is of great significance to develop new crystal forms of nicotinamide derivatives which are more advantageous to use in drug processing and pharmaceutical compositions, and to provide more qualitative and quantitative information for the rapeutic effect studies of solid drug.